Copper-Mediated Synthesis of 1,2,3-Triazoles from N-Tosylhydrazones and Anilines


  • We gratefully acknowledge the National Basic Research Program of China (no. 2011CB936003), the Natural Science Foundation of China (no. 2107216 and no. 21272205), and the Program for the Zhejiang Leading Team of Science and Technology Innovation for their financial support.


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NNNifty targets: In a straightforward copper-mediated synthesis of 1,4-disubstituted and 1,4,5-trisubstituted 1,2,3-triazoles, readily available aniline and N-tosylhydrazone substrates underwent cyclization through C[BOND]N and N[BOND]N bond formation (see scheme; Piv=pivaloyl, Ts=p-toluenesulfonyl). This method enables the preparation of 1,2,3-triazoles with high efficiency under mild conditions without the use of azides.